凝血酶受体拮抗剂——Vorapaxar的安全性和有效性

Safety and Efficacy of Thrombin Receptor Antagonist——Vorapaxar

随着社会的飞速发展,人们的物质生活得到极大的改善,生活习惯也发生了改变,同时,也导致了心脑血管疾病发病率和病死率的升高。在心脑血管疾病的发生过程中,血小板的活化与聚集扮演着十分重要的角色。现有的抗血小板药物,包括影响花生四烯酸代谢的药物(阿司匹林)、增高环磷酸腺苷水平的药物(贝前列素、西洛他唑等)、腺苷二磷酸受体拮抗剂(氯吡格雷等)和纤维蛋白原受体拮抗剂(替罗非班、埃替非班、阿昔单抗等),使心脑血管不良事件发生率明显减少,但仍有一部分人群在接受现有抗血小板药物治疗时发生心脑血管不良事件,而且伴有不同程度的出血。为了减少心脑血管不良事件,同时降低出血风险,对抗血小板药物提出了更高的要求。血小板蛋白酶激活受体-1拮抗剂——Vorapaxar,理论上被认为不干扰正常血小板保护性的凝血途径,被期待成为不增加出血风险但具备良好的降低血管事件的新型抗血小板药物,现就其安全性和有效性进行回顾性研究。

With the rapid development of society,people＇＇s material life has greatly improved,life habits have changed and at the same time,the incidence of cardiovascular disease and mortality rates have increased.The activation and aggregation of platelets play an important role in the occurrence of cardiovascular and cerebrovascular diseases.In the existing antiplatelet drugs,cardiovascular adverse events were significantly reduced,but there are still a number of people in existing treatment of antiplatelet drugs during cardiovascular adverse events,but with different degrees of bleeding.Such antiplatelet drugs include drugs that affect four arachidonic acid metabolism（aspirin）,increased cyclic adenosine monophosphate levels of drugs（beraprost,cilostazol,etc.）,ADP receptor antagonist（clopidogrel） and fibrinogen receptor antagonist（tirofiban,ethiopia,abciximab for non-class monoclonal antibody）.In order to reduce adverse cardiovascular and cerebrovascular events,while reducing the risk of bleeding,a higher requirement is put forward.Platelet protease activated receptors-1,antagonist vorapaxar,theorized that does not interfere with normal platelet protection of the coagulation pathway,is expected to be a new antiplatelet agent that does not increase the risk of bleeding but has a good rate of lowering vascular events.This paper makes a retrospective study on its safety and effectiveness.